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γ-氨基丁酸及其衍生物的药理特性。IV. 芳基γ-氨基丁酸衍生物及其相应的内酰胺。

Pharmacological properties of gamma-animobutyric acid and it derivatives. IV. Aryl gaba derivatives and their respective lactams.

作者信息

Chojnacka-Wójcik E, Hano J, Sieroslawska J, Sypniewska M

出版信息

Arch Immunol Ther Exp (Warsz). 1975;23(6):733-46.

PMID:1241266
Abstract

Pharmacological properties of alpha-(AFG), beta-(FG) and gamma-(GFM) phenyl-substituted derivatives of GABA and their respective lactams (FP, FL, FM) were studied in rats and mice. All studied compounds diminished spontaneous and pharmacologically potentiated motility, lowered body temperature of mice, and weakened conditioned reflexes in rats. Some of the compounds (AFG, FG, FP) diminished activity of rats in the open-field test and symptoms of amphetamine- (AFG, FG, FP, FL, FM) and apomorphine-induced stereotypy (FL, FG). FG evoked catalepsy and potentiated chlorpromazine catalepsy in mice. The compounds potentiated action of narcotic and subthreshold doses of barbiturates and ethanol, had analgesic properties, and potentiated analgesic action of morphine. The most active and least toxic compound was beta-phenyl-gamma-aminobutyric acid (FG).

摘要

研究了γ-氨基丁酸(GABA)的α-(AFG)、β-(FG)和γ-(GFM)苯基取代衍生物及其各自的内酰胺(FP、FL、FM)在大鼠和小鼠体内的药理特性。所有研究的化合物均能减少自发运动和药理增强的运动,降低小鼠体温,并减弱大鼠的条件反射。一些化合物(AFG、FG、FP)在旷场试验中降低了大鼠的活动,以及苯丙胺(AFG、FG、FP、FL、FM)和阿扑吗啡诱导的刻板行为(FL、FG)的症状。FG在小鼠中诱发了僵住症并增强了氯丙嗪引起的僵住症。这些化合物增强了麻醉剂量和阈下剂量巴比妥类药物及乙醇的作用,具有镇痛特性,并增强了吗啡的镇痛作用。活性最高且毒性最小的化合物是β-苯基-γ-氨基丁酸(FG)。

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